In this study, pillar[5]arene containing ten terminal alkynyl-functional group was prepared and carried out an optimization procedure for target molecule with using 5-hydroxyquinoline molecule known with biological activity. The novel molecule was named as iso-QP[5] and characterized by FT-IR, melting point, NMR, elemental analysis, and mass spectroscopy. The aim was to evaluate the anticancer effects of iso-QP[5] on MCF7 human breast cancer cells. The IC₅₀ dose of iso-QP[5] in MCF7 cells was found to be 25 µM for 24 h using XTT assay. Expressions of eight genes for apoptosis were determined by qPCR. The results showed a significant increase in the expression of BAX, CASP3, CASP9, CYCS, and P53 genes after treatment with iso-QP[5] in MCF7 cells. However, iso-QP[5] treatment significantly decreased expression of BCL2 and CASP8 genes. It is concluded that novel molecule iso-QP[5] caused apoptosis by regulating genes that are important in apoptosis in human breast cancer cells.

中文翻译：

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新型基于分子[5]芳烃的多喹啉单元的合成及抗癌作用的评价

在这项研究中，制备了具有十个末端炔基官能团的支柱[5]芳烃，并使用具有生物活性的5-羟基喹啉分子对目标分子进行了优化。这种新型分子被命名为iso-QP [5]，并通过FT-IR，熔点，NMR，元素分析和质谱表征。目的是评估iso-QP [5]对MCF7人乳腺癌细胞的抗癌作用。XTT分析显示，在MCF7细胞中，iso-QP [5]的IC ₅₀剂量在24小时内为25 µM。通过qPCR确定八个细胞凋亡基因的表达。结果表明在表达的增加显著BAX，CASP3，CASP9，CYCS，和P53iso-QP [5]处理后的MCF7细胞中的基因。但是，iso-QP [5]处理显着降低了BCL2和CASP8基因的表达。结论是，新型分子iso-QP [5]通过调节在人类乳腺癌细胞凋亡中重要的基因引起细胞凋亡。